435300 LFM-A13 - CAS 62004-35-7 - Calbiochem

435300
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₁H₈Br₂N₂O₂62004-35-7

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435300-5MGCN
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      Plastic ampoule 5 mg
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      Description
      OverviewA potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
      Catalogue Number435300
      Brand Family Calbiochem®
      Synonymsα-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton's Tyrosine Kinase Inhibitor I
      References
      ReferencesUckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
      Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
      Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
      Product Information
      CAS number62004-35-7
      ATP CompetitiveY
      FormLight brown solid
      Hill FormulaC₁₁H₈Br₂N₂O₂
      Chemical formulaC₁₁H₈Br₂N₂O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetHuman Bruton's Tyrosine Kinase (BTK)
      Primary Target IC<sub>50</sub>17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      LFM-A13 - CAS 62004-35-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      435300

      References

      Reference overview
      Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
      Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
      Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.

      Citations

      Title
    • Sarah L Doyle, Caroline A Jefferies and Luke A O'Neill. (2005) Bruton's tyrosine kinase is involved in p65-mediated transactivation and phosphorylation of p65 on serine 536 during NF-B activation by LPS. Journal of Biological Chemistry 280, 23496-23501.
    • Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision12-January-2010 RFH
      Synonymsα-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton's Tyrosine Kinase Inhibitor I
      DescriptionA potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
      FormLight brown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number62004-35-7
      Chemical formulaC₁₁H₈Br₂N₂O₂
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (200 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesUckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
      Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
      Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
      Citation
    • Sarah L Doyle, Caroline A Jefferies and Luke A O'Neill. (2005) Bruton's tyrosine kinase is involved in p65-mediated transactivation and phosphorylation of p65 on serine 536 during NF-B activation by LPS. Journal of Biological Chemistry 280, 23496-23501.